JJ1
JJ1 is a selective α-thrombin inhibitor with a Ki of 0.019 μM. JJ1 directly binds to the active site of α-thrombin to block its catalytic activity. JJ1 exhibits antithrombotic effects and prolongs activated partial thromboplastin time, prothrombin time, and tail bleeding time in mice. JJ1 can be used for the research of thrombotic diseases.
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- No. CAS: 1225170-16-0
- Fòrmula: C18H19N5
- Peso molecular:305.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
α-thrombin 0.019 μM (Ki) |
In Vitro
JJ1 (1 h) potently and selectively inhibits α-thrombin with a Ki value of 0.019 μM, and exhibits a selectivity of over 10000-fold against other tested human serine proteases[1].
JJ1 (0-2.5 μM; 1 min) inhibits the amidolytic activity of thrombin in a dose-dependent manner, with an IC50 value of 0.15 μM[1].
JJ1 (0-5 μM; 0-60 min) inhibits the activity of human thrombin bound to blood clots in a dose-dependent manner, with an IC50 of 2.45 μM[1].
JJ1 (0.5-5 μM; 1-10 min) dose-dependently inhibits thrombin-induced aggregation of washed platelets, with significant inhibitory effects observed at concentrations ≥0.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC | T1/2 |
|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 6.1 μg·h/mL | 3.1 h |
In Vivo
JJ1 (0.31-3.06 μg/mouse; intravenous injection; single administration) dose-dependently prolongs tail bleeding time, ex vivo activated partial thromboplastin time (aPTT), and ex vivo prothrombin time (PT) in healthy male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-7 weeks old, 27 g, ferric chloride-induced arterial thrombosis model)[1]
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Dosage:0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
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Administration:i.v.; single dose
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Result:Significantly slowed thrombus growth.
Reduced thrombus size score.
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Animal Model:C57BL/6 (male, 6-7 weeks old, 27 g)[1]
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Dosage:0.31 μg/mouse; 0.61 μg/mouse; 1.23 μg/mouse; 3.06 μg/mouse
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Administration:i.v.; single dose
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Result:Prolonged tail bleeding time to 37.2 seconds at 0.61 μg/mouse, 44.8 seconds at 1.23 μg/mouse, and 52.2 seconds at 3.06 μg/mouse (control time was 30.2 seconds).
Prolonged ex vivo aPTT to 40.1 seconds at 0.61 μg/mouse, 49.4 seconds at 1.23 μg/mouse, and 55.8 seconds at 3.06 μg/mouse (control aPTT was 32.1 seconds).
Prolonged ex vivo PT to 17.2 seconds at 0.61 μg/mouse, 22.3 seconds at 1.23 μg/mouse, and 26.8 seconds at 3.06 μg/mouse (control PT was 12.0 seconds).
Chemical Information
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No. CAS 1225170-16-0
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Peso molecular 305.39
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Fòrmula C18H19N5
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SMILES
N=1C=CC(=CC1)NC=2N=C3C=CC=CC3=C(N2)NC4CCCC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JJ1 Related Classifications
HY-165360 Related Classifications
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Keywords
- JJ1
- 1225170-16-0
- JJ 1
- JJ-1
- Thrombin
- serine proteases
- collagen + epinephrine-induced acute pulmonary thrombosis model
- human α-thrombin
- human plasma
- endothelial cells
- thrombotic disorders
- ferric chloride-induced arterial thrombosis model
- human umbilical vein endothelial cells
- C57BL/6 mice
- human platelets
- Inhibitor
- inhibitor
- inhibit